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Assay Detail

CHEMBL4416374

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Functional
Allosteric modulator activity at human CB1 receptor expressed in CHO-RD-HGA16 cells co-expressing Galpha16 assessed as suppression of 100 nM CP55,940-induced calcium mobilization pre-incubated for 15 mins by Calcium 5 dye based FLIPR assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
Nguyen T, Gamage TF, Decker AM, Barrus D, Langston TL, Li JX, Thomas BF, Zhang Y.
J Med Chem (2019) 62 : 9806 -9823
PubMed 31596583 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.97 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4527602 1 8.17
CHEMBL4464917 1 7.68
CHEMBL4590582 1 7.66
CHEMBL4584483 1 7.51
CHEMBL3341861 1 7.48
CHEMBL4528445 1 7.43
CHEMBL4572697 1 7.41
CHEMBL4544453 1 7.40
CHEMBL4452850 1 7.40
CHEMBL4565127 1 7.37
CHEMBL4438047 1 7.32
CHEMBL4442623 1 7.24
CHEMBL4542852 1 7.22
CHEMBL4513477 1 7.21
CHEMBL4591294 1 7.10
CHEMBL4581327 1 7.10
CHEMBL4450625 1 7.05
CHEMBL4474515 1 7.04
CHEMBL4472252 1 6.97
CHEMBL4580323 1 6.97
CHEMBL4450873 1 6.96
CHEMBL4443032 1 6.81
CHEMBL4577814 1 6.63
CHEMBL4539271 1 6.54
CHEMBL4577767 1 6.46
CHEMBL4554290 1 6.30
CHEMBL4443540 1 5.91
CHEMBL4542455 1 5.90
CHEMBL4457227 1 5.45
CHEMBL4475934 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4527602 IC50 = 6.8 nM 8.17
CHEMBL4464917 IC50 = 21.0 nM 7.68
CHEMBL4590582 IC50 = 22.0 nM 7.66
CHEMBL4584483 IC50 = 31.0 nM 7.51
CHEMBL3341861 IC50 = 33.0 nM 7.48
CHEMBL4528445 IC50 = 37.0 nM 7.43
CHEMBL4572697 IC50 = 39.0 nM 7.41
CHEMBL4544453 IC50 = 40.0 nM 7.40
CHEMBL4452850 IC50 = 40.0 nM 7.40
CHEMBL4565127 IC50 = 43.0 nM 7.37
CHEMBL4438047 IC50 = 48.0 nM 7.32
CHEMBL4442623 IC50 = 58.0 nM 7.24
CHEMBL4542852 IC50 = 60.0 nM 7.22
CHEMBL4513477 IC50 = 61.0 nM 7.21
CHEMBL4591294 IC50 = 79.0 nM 7.10
CHEMBL4581327 IC50 = 79.0 nM 7.10
CHEMBL4450625 IC50 = 89.0 nM 7.05
CHEMBL4474515 IC50 = 92.0 nM 7.04
CHEMBL4472252 IC50 = 108.0 nM 6.97
CHEMBL4580323 IC50 = 107.0 nM 6.97
CHEMBL4450873 IC50 = 111.0 nM 6.96
CHEMBL4443032 IC50 = 156.0 nM 6.81
CHEMBL4577814 IC50 = 233.0 nM 6.63
CHEMBL4539271 IC50 = 292.0 nM 6.54
CHEMBL4577767 IC50 = 345.0 nM 6.46
CHEMBL4554290 IC50 = 501.0 nM 6.30
CHEMBL4443540 IC50 = 1220.0 nM 5.91
CHEMBL4542455 IC50 = 1270.0 nM 5.90
CHEMBL4457227 IC50 = 3530.0 nM 5.45
CHEMBL4475934 IC50 = 3880.0 nM 5.41
CHEMBL4468436 IC50 > 10000.0 nM -